| CAS NO: | 57477-39-1 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 230.31 |
| Cas No. | 57477-39-1 |
| Formula | C14H18N2O |
| Solubility | Soluble in DMSO |
| Chemical Name | 3-(1-methylpiperidin-4-yl)-1H-indol-5-ol |
| Canonical SMILES | CN1CCC(CC1)C2=CNC3=C2C=C(C=C3)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
BRL-54443是一种有效的5-HT1E和5HT1F受体激动剂(pEC50 = 8.5和8.6),选择性是人克隆5-HT1A的30多倍,是其他5-HT和多巴胺受体的50多倍[1].
5-HT受体是一种神经系统中5-羟色胺(血清素)的G-蛋白偶联受体.它也是多种生物碱和精神活性物质的受体.
在使用大鼠脑皮脂膜的研究中,BRL-54443导致[3H]-5-HT的双相抑制[1].在C57BL/6J小鼠主动脉中,BRL 54443在Ketanserin(5-HT2A和5-HT2C受体拮抗剂)存在下可引起收缩[3].
在Sprague Dawley大鼠中,BRL- 54443以剂量3 mg/kg和5 mg/kg给药,减少自主运动行为[2].BRL-4443也刺激大鼠的嗅觉行为[2].在恒压研究中,恒压下监测猫的胃容量,BRL-54443引起剂量依赖性的胃容量增加[4].
参考文献：
1. A.M. Brown, K. Avenell, T J. Young et al. BRL 54443, a potent agonist with selectivity for human cloned 5-HT1E and 5-HT1F receptors. 1998. Br.J.Pharmacol. 123 233P.
2. S. Lightowler, T. Stean, N. Upton et al. Effect of BRL 54443 (3-(1-methylpiperidin-4-yl)-1H-indol-5-ol), a 5-HT1E/1F receptor agonist, on general behaviour and maximal electroshock seizure threshold in the rat. 1998. Br.J.Pharmacol. 123 237P.
3. McKune CM, Watts SW. Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95.
4. Janssen P, Tack J, Sifrim D et al. Influence of 5-HT1 receptor agonists on feline stomach relaxation. Eur J Pharmacol. 2004 May 25;492(2-3):259-67.
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